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DERIVADOS DE 1,3-TIAZOLIDINA-2,4-DIONA CON ACTIVIDAD SOBRE QUINASAS PIM-1 Y/O PIM-2 Y/O PIM-3
专利权人:
ASTRAZENECA AB
发明人:
DAKIN, LESLIE,DOWLING, JAMES EDWARD,LAMB, MICHELLE,READ, JON,SU, QIBIN,ZHENG, XIAOLAN
申请号:
PE0012212010
公开号:
PE03042012A1
申请日:
2009.07.02
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Referring to a compound derived from 1.3 - thiazolidine-2,4-dione of formula (i), wherein R1 is a Group carbociclilo as ciclopropilo, Cyclopentyl, Cyclohexyl, among others, an aryl Group as phenyl or naphthyl, or a group heterociclilo r1 can be optionally substituted by one or more R2 Where R2 is alkyl, halogen, alkyl of C1 - C6 C1 - C6 Halogenated alkyl, amino, C1 - C6 amino2amino (C1 - C6 alkyl), among others.Preferred compounds are: 5 - ({2 - [(3S) - 3 - aminopiperidin - triazin-1-yl] - 3 - Chloro - 5 - (trifluoromethyl) phenyl} metilideno - 1.3 - tiazolidona - 2.4 - dione, 5 - 3 - Chloro - ({2 - [(3S) - 3 - (dimethylamino) pyrrolidin-1-yl] - 5 - (trifluoromethyl) phenyl) - 1,3 -} metilideno thiazolidine-2,4-dione, N - (4 - [3 - (dimethylamino) pyrrolidin-1-yl] - 3 - [(Z) - (2.4 - [- 5 - 1.3 - tiazolidin - ylidene) methyl] phenyl] acetamide, among others.It also relates to a method of Preparation. These compounds are inhibitors or modulators of Enzyme activity or function of the Protein Kinase pim-1 and \/ or pim-2 and \/ or pim-3 and are useful in the treatment of diseases mediated by these Kinases, preferably, cancerREFERIDA A UN COMPUESTO DERIVADO DE 1,3-TIAZOLIDINA-2,4-DIONA DE FORMULA (I), DONDE R1 ES UN GRUPO CARBOCICLILO TAL COMO CICLOPROPILO, CICLOPENTILO, CICLOHEXILO, ENTRE OTROS, UN GRUPO ARILO TAL COMO FENILO O NAFTILO, O UN GRUPO HETEROCICLILO R1 PUEDE ESTAR OPCIONALMENTE SUSTITUIDO POR UNO O MAS R2, DONDE R2 ES HALOGENO, ALQUILO C1-C6, ALQUILO C1-C6 HALOGENADO, AMINO, ALQUIL C1-C6 AMINO, (ALQUIL C1-C6)2AMINO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 5-({2-[(3S)-3-AMINOPIPERIDIN-1-IL]-3-CLORO-5-(TRIFLUOROMETIL) FENIL}METILIDENO-1,3-TIAZOLIDONA-2,4-DIONA, 5-({3-CLORO-2-[(3S)-3-(DIMETILAMINO)PIRROLIDIN-1-IL]-5-(TRIFLUOROMETIL)FENIL}METILIDENO)-1,3-TIAZOLIDINA-2,4-DIONA, N-{4-[3-(DIMETILAMINO)PIRROLIDIN-1-IL]-3-[(Z)-(2,4-DIOXO-1,3-TIAZOLIDIN-5-ILIDENO)METIL]FENIL}ACETAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPU
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